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首页> 美国卫生研究院文献>Molecules >trans-Caryophyllene a Natural Sesquiterpene Causes Tracheal Smooth Muscle Relaxation through Blockade of Voltage-Dependent Ca2+ Channels
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trans-Caryophyllene a Natural Sesquiterpene Causes Tracheal Smooth Muscle Relaxation through Blockade of Voltage-Dependent Ca2+ Channels

机译：反式石竹烯一种天然的倍半萜烯通过阻断电压依赖性Ca 2+通道引起气管平滑肌松弛

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trans-Caryophyllene is a major component in the essential oils of various species of medicinal plants used in popular medicine in Brazil. It belongs to the chemical class of the sesquiterpenes and has been the subject of a number of studies. Here, we evaluated the effects of this compound in airway smooth muscle. The biological activities of trans-caryophyllene were examined in isolated bath organs to investigate the effect in basal tonus. Electromechanical and pharmacomechanical couplings were evaluated through the responses to K+ depolarization and exposure to acetylcholine (ACh), respectively. Isolated cells of rat tracheal smooth muscle were used to investigate trans-caryophyllene effects on voltage-dependent Ca2+ channels by using the whole-cell voltage-clamp configuration of the patch-clamp technique. trans-Caryophyllene showed more efficiency in the blockade of electromechanical excitation-contraction coupling while it has only minor inhibitory effect on pharmacomechanical coupling. Epithelium removal does not modify tracheal smooth muscle response elicited by trans-caryophyllene in the pharmacomechanical coupling. Under Ca2+-free conditions, pre-exposure to trans-caryophyllene did not reduce the contraction induced by ACh in isolated rat tracheal smooth muscle, regardless of the presence of intact epithelium. In the whole-cell configuration, trans-caryophyllene (3 mM), inhibited the inward Ba2+ current (IBa) to approximately 50% of control levels. Altogether, our results demonstrate that trans-caryophyllene has anti-spasmodic activity on rat tracheal smooth muscle which could be explained, at least in part, by the voltage-dependent Ca2+ channels blockade.
机译：反式石竹烯是巴西流行医学中使用的各种药用植物精油中的主要成分。它属于倍半萜的化学类别，并且已经成为许多研究的主题。在这里，我们评估了该化合物对气道平滑肌的作用。在分离的浴器官中检查了反式石竹烯的生物学活性，以研究其对基底突的影响。通过对K + 去极化和暴露于乙酰胆碱（ACh）的响应分别评估了机电耦合和药物耦合。采用膜片钳技术的全细胞电压钳构型，通过分离大鼠气管平滑肌细胞，研究反叶石竹烯对电压依赖性Ca 2 + 通道的影响。反式石竹烯在阻断机电激发-收缩偶联方面显示出更高的效率，而对药效机械偶联仅具有较小的抑制作用。去除上皮并不会改变在药效机械偶联中由反式石竹烯引起的气管平滑肌反应。在无Ca 2 + 的条件下，无论是否存在完整的上皮细胞，预先暴露于反式石竹烯都不会降低ACh诱导的离体大鼠气管平滑肌的收缩。在全细胞配置中，反石竹烯（3 mM）抑制向内的Ba 2 + 电流（IBa）达到对照水平的约50％。总之，我们的结果表明反式石竹烯对大鼠气管平滑肌具有抗痉挛活性，这至少可以部分地由电压依赖性Ca 2 + 通道的阻断来解释。

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